Name: Taselisib (GDC 0032)
Brand: Selleck Chemicals
SKU: S7103
Rating: 5 (39 reviews)

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other PI3K Inhibitors	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
human MOLM16 cells	Proliferation assay		72 h		Antiproliferative activity against human MOLM16 cells after 72 hrs by Cell Titer-Blue assay
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	460.53	Formula	C₂₄H₂₈N₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1282512-48-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RG7604			Smiles	CC1=NN(C(=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)C5=CN(N=C5)C(C)(C)C(=O)N)C(C)C

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (151.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.600mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 92 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.460mg/ml (1.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	A beta isoform-sparing PI3K inhibitor.
Targets/IC₅₀/Ki	PI3Kδ (Cell-free assay) 0.12 nM(Ki) PI3Kα (Cell-free assay) 0.29 nM(Ki) PI3Kγ (Cell-free assay) 0.97 nM(Ki) PI3Kβ (Cell-free assay) 9.1 nM(Ki) C2β (Cell-free assay) 292 nM hVps34 (Cell-free assay) 374 nM
In vitro	GDC-0032 is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ isoforms, with 30 fold less inhibition of the PI3K β isoform relative to the PI3Kα isoform. Preclinical data show that GDC-0032 has increased activity against PI3Kα isoform (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM.
Kinase Assay	Characterisation of Biochemical and Cellular Activity In Vitro
Kinase Assay	Enzymatic activity of the class I PI3K isoforms is measured using a fluorescence polarisation assay that monitors formation of the product 3,4,5-inositoltriphosphate molecule as it competes with fluorescently labelled PIP3 for binding to the GRP-1 pleckstrin homology domain protein. An increase in phosphatidyl inositide-3-phosphate product results in a decrease in fluorescence polarisation signal as the labelled fluorophore is displaced from the GRP-1 protein binding site. Class I PI3K isoforms are expressed and purified as heterodimeric recombinant proteins. Tetramethylrhodamine-labelled PIP3 (TAMRA-PIP3), di-C8-PIP2, and PIP3 detection reagents are purchased from Echelon Biosciences. PI3Kα is assayed under initial rate conditions in the presence of 10 mM Tris (pH 7.5), 25 μM ATP, 9.75 μM PIP2, 5% glycerol, 4 mM MgCl₂, 50 mM NaCl, 0.05% (v/v) Chaps, 1 mM dithiothreitol, and 2% (v/v) DMSO at 60 ng/mL. After assay for 30 min at 25 °C, reactions are terminated with a final concentration of 9 mM EDTA, 4.5 nM TAMRA-PIP3, and 4.2 μg/mL GRP-1 detector protein before reading fluorescence polarisation on an Envision plate reader. IC50 values are calculated from the fit of the dose-response curves to a 4-parameter equation. Each reported value is an average of three experiments, and all have a standard deviation less than one geometric mean.
In vivo	GDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t_1/2 of 40 hours. The combination of GDC-0032 enhances activity resulting in tumour regressions and tumour growth delay (91% tumour growth inhibition (TGI)). In addition, the combination of GDC-0032 enhances the efficacy in vivo (102%TGI for GDC-0032).
References	[1] https://pubmed.ncbi.nlm.nih.gov/23662903/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Cyclin D1 / Cyclin E / Cleaved PARP / p-AKT / pPRAS40 / p-mTOR / pp70S6K / BRCA1 / c-Myc		27382432
Growth inhibition assay	Cell viability		27382432

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02785913	Completed	Recurrent Squamous Cell Lung Carcinoma\|Stage IV Squamous Cell Lung Carcinoma	SWOG Cancer Research Network\|National Cancer Institute (NCI)	November 2014	Phase 2
NCT01967966	Completed	Healthy Volunteer	Genentech Inc.	November 2013	Phase 1
NCT01814709	Completed	Healthy Volunteer	Genentech Inc.	April 2013	Phase 1

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Handling Instructions

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Taselisib (GDC 0032) PI3K inhibitor

Chemical Structure

Molecular Weight: 460.53